SEP 24, 2014 05:00 AM PDT

Exploring macrocycles for drug discovery: Novel lead series for challenging protein-protein interactions

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  • Chief Scientific Officer, Ensemble Therapeutics

      Nick joined Ensemble Therapeutics as the Chief Scientific Officer in May 2006. In his role as CSO, Nick heads up the firm's drug discovery program investigating the rapid synthesis of macrocycles using DNA-programmed chemistry, as drug candidates for disease relevant protein-protein and protease targets.After working as a medicinal chemist for Glaxo, Nick joined Pfizer in Sandwich, England in 1984. He worked initially in cardiovascular disease, and is an inventor on patents for the neutral endopeptidase inhibitor candoxatrilat. Later he led the chemistry team on cGMP PDE inhibitors for angina and erectile dysfunction, and is an inventor on patents for Viagra. Subsequently, Nick established Pfizer's combinatorial chemistry group and authored several related papers and a textbook. He also managed the high throughput screening group and materials management, and played a key role in the global integration of the Pfizer, Warner-Lambert and Pharmacia compound collections. In 2003 Nick moved to the Pfizer Research Technology Center in Cambridge, Massachusetts, to lead the Chemical Sciences group investigating new targets for drug discovery and new chemistry technologies.  

    Macrocycles offer a new structural class that has the potential to address challenging protein-protein interaction targets and still present attractive drug-like properties including cell membrane penetration and oral bioavailability. Indeed a number of orally active drugs based on naturally occurring macrocycles provide a compelling precedent for this argument. Ensemble have used DNA-programmed chemistry to make over 10 million synthetic macrocycles in a library format that permits rapid and efficient screening against therapeutically relevant targets. The talk will present successful Ensemble case studies with XIAP antagonists for oncology, and IL17 antagonists for inflammatory disease.

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